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In summary P P macrocyclization proved to be
2022-08-17
In summary, P2-P4 macrocyclization proved to be an effective strategy to drive activity in this series of HCV NS3 protease inhibitors while microsomal stability was enhanced by the introduction of steric bulk along the tether. This modification augmented the previously-described tactic of improving
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Previous reports have implicated the guanylin
2022-08-17
Previous reports have implicated the guanylin/GC-C signalling system as being important in osmoregulation in fish, especially in euryhaline species such as the eel which migrate between freshwater (FW) and seawater (SW) environments at different stages of their life cycle (Comrie et al., 2001a, Comr
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It has been shown that GPR receptors coupled
2022-08-17
It has been shown that GPR55 receptors coupled to G12/13 proteins down-regulate reactive oxygen species (ROS) production and degranulation in human neutrophils [9]. MCs degranulation stimulated by IgE/Ag also requires the generation of ROS [64]; therefore, the possibility to explore the inhibitory a
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The first described synthetic FFA active agonist GW
2022-08-17
The first described synthetic FFA1 active agonist, GW9508 (4- [(3-phenoxyphenyl)methyl]amino benzenepropanoic acid), was immediately shown to also activate FFA4, although with some 100-fold lower potency [38]. Therefore, in the initial absence of FFA4-selective synthetic agonist ligands, GW9508 was
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Introduction The West syndrome or epilepsy with
2022-08-17
Introduction The West syndrome or epilepsy with epileptic spasms (ES) is an epileptic encephalopathy in early infancy with probable seizure-related developmental regression. According to the United Kingdom Infantile Spams Study (UKISS), common causes of infantile spasms include hypoxic-ischemic enc
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The development of immobilization techniques for
2022-08-17
The development of immobilization techniques for β-glucosidase offers a potential way to enable its reuse several times [13]. The aim of immobilization is to trap the enzyme within or on the surface of an insoluble material with retention of its catalytic activity [14]. The immobilization strategy a
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br Conclusions Temporally controlled disruption of Gcgr reve
2022-08-17
Conclusions Temporally-controlled disruption of Gcgr reveals a lack meaningful contribution to the improvement of glycemic control in insulinopenic conditions attributable to the intrinsic loss of GCGR signaling. On the other hand, these data highlight the importance of compensatory systems, incl
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br Acknowledgements br Introduction Muscle FBPase is very
2022-08-16
Acknowledgements Introduction Muscle FBPase is very sensitive to AMP inhibition and in the presence of physiological concentrations of this effector in muscle fibres FBPase should be almost completely inactive [1], [2]. Recently, we have presented evidence that, in vitro, muscle aldolase binds
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br Conclusion H R H R and H R mRNAs
2022-08-16
Conclusion H1R, H2R, and H3R mRNAs were expressed in rat OE. Moreover, these three histamine receptors were present in the cytoplasm of ORNs in OE. This is the first report of the expression and localization of histamine receptors in mammalian OE. These findings indicate that histamine may play a
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br Conclusion Leukocytes adhesion to
2022-08-16
Conclusion Leukocytes adhesion to endothelial cells is one of the most critical event in the inflammatory response. In presented paper using a relevant model of adhesion we have demonstrated that histamine influence eosinophils adhesion to endothelium. This effect appears to be mediated by H4 his
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In recent years the Hippo signaling pathway has emerged
2022-08-16
In recent years, the Hippo signaling pathway has emerged as an important regulator balancing cell proliferation and differentiation [[5], [6], [7]]. The pathway components, first described in the fruit fly Drosophila melanogaster, are highly conserved across different phyla [6]. The signaling pathw
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br Regulation of HO expression under conditions
2022-08-16
Regulation of HO-1 expression under conditions of ischemic cardiac damage Heart is a vital organ with high metabolic demand, rich in mitochondria and it is very vulnerable to oxidative damage [85]. Disruption in coronary blood flow following MI leads to hypoxia (a reduction in the amount of avail
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Starting from the hypothesis that the linker portion of
2022-08-16
Starting from the hypothesis that the linker portion of the inhibitor molecules does not necessarily require the presence of an alcohol/ether or a carbonyl group, the same research group performed another scaffold hopping analysis, obtaining 1500 new compounds as potentially active HO-1 inhibitors [
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LY364947 australia Thus our data demonstrate that
2022-08-15
Thus, our data demonstrate that polymorphisms of GSTP1-1 differentially mediate activation of Prdx6 peroxidase activity, providing a platform to imply that contingent upon their GSTP genotype, individuals will have significant differences in mounting an antioxidant response, particularly affecting p
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BCA Protein Quantitation Kit Disrupting the dialog between m
2022-08-15
Disrupting the dialog between microbiota and the host, especially at the level of mucosal immunology, is expected to have profound effects on disease development. By using the AOM+DSS model of colitis-associated CRC, Singh et al. (2014) showed that development of inflammation and CRC are exacerbated
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